Acute toxicity of 3-(2-, 3-fluorophenyl)-6-(aryl-, hetaryl)-[1,2,4]triazole[3,4-b][1,3,4]thiadiazoles

The treatment of infectious diseases is a challenging issue faced by the medical community. The emergence of drug-resistant strains of bacteria and fungi is a major concern. Researchers and medical professionals are working to develop new and innovative treatments for infectious diseases. Schiff bases are one a promising class of compounds. In this work, new derivatives were obtained of the 4-amino-5-(3-fluorophenyl)-2,4-dihydro-3H-1,2,4-triazole-3-thione reaction, with corresponding benzaldehydes with various substituents at position 4. The antibacterial and antifungal activities of all synthesized compounds were tested. Several new substances have shown moderate antifungal activity against Candida spp. The highest activity directed against C. albicans was shown by compound RO4, with a 4-methoxyphenyl moiety and an MIC value of 62.5 µg/mL. In order to check the toxicity of the synthesized compounds, their effect on cell lines was examined. Additionally, we tried to elucidate the mechanism of the antibacterial and antifungal activity of the tested compounds using molecular docking to topoisomerase IV, D-Alanyl-D-Alanine Ligase, and dihydrofolate reductase.

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“…5-(3-fluorophenyl)-4-[(4-methoxybenzylidene)amino]-2,4-dihydro-3 H -1,2,4-triazole-3-thione (RO4) [ 51 ] CAS 2362542-60-5…”

Section: Methodsmentioning

confidence: 99%

Synthesis and Biological Evaluation of New Schiff Bases Derived from 4-Amino-5-(3-fluorophenyl)-1,2,4-triazole-3-thione

et al. 2023

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“…Numerous publications by various scientific teams from around the world have demonstrated the high reactivity of 1,2,4-triazole derivatives, as well as their low toxicity [6,10], and a wide range of possibilities for their use as potential biologically active compounds [7][8][9]. Promising properties of some 1,2,4-triazole derivatives, which are used as effective plant growth regulators, have been described in [8,11]. It is worth emphasizing the possibility of using 1,2,4-triazole derivatives as veterinary drugs [9,10].…”

Section: Original Researchmentioning

confidence: 99%

“…the 3-(2-,3-fluorophenyl)-6-(aryl-,heteryl)-[1,2,4] triazolo[3,4-b][1,3,4] thiadiazoles, four exceed the reference diuretic hypothiazide (2, 4, 5, 6, Table1), and 3-(2-fluorophenyl)-6-(phenyl)-[1,2,4]triazole[3,4-b][1,3,4]thiadiazole (1), 3-(3-fluorophenyl)-6-(3-methoxyphenyl)-[1,2,4] triazole[3,4-b][1,3,4]thiadiazole (7) and 3-(3-fluorophenyl)-6-(2-bromo-4-fluorophenyl)-[1,2,4]triazole[3,4-b] [1,3,4]thiadiazole(8) approximate by activity to furosemide. Regarding the activity of 3-(2-,3-fluorophenyl)-6-R 2 -7H[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines(9)(10)(11)(12)(13)(14) Table …”

mentioning

confidence: 99%

Diuretic activity of some 4- and 3-thio-substituted 1,2,4-triazoles with fluorophenyl fragments

et al. 2023

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Diuretics increase the volume of urine and sodium excretion, and therefore are often used to remove excess fluid from the body during various diseases, including hypertension, heart and kidney failure, nephrotic syndrome, cirrhosis, etc. Until now, a wide range of diuretics is known, but none of them is completely safe and has a number of side effects. The aim of the work is to investigate the diuretic activity of 1,2,4-triazole derivatives containing fluorophenyl substituents at the fifth position of the 1,2,4-triazole fragment, as well as to establish the relationship between “chemical structure and diuretic action” among derivatives 1,2,4-triazole. Materials and methods. To study the effect on kidney function, six groups of animals with seven rats each were used. When studying water diuresis, rats were kept on a constant diet with free access to water. Before water loading (5 % of body weight), rats were fasted for 2 hours without food and water. Since all tested compounds were insoluble in water, they were administered orally as an aqueous suspension stabilized with Tween-80. The compounds were administered at a dose of 1/10 LD50. Results. The diuretic activity of 28 new compounds of a number of substituted 1,2,4-triazole-3-thiols, which according to their chemical structure belong to different classes of compounds, was investigated. Conclusions. Analysis of the results of diuretic activity indicates that there are a number of compounds whose activity is higher than hypothiazide, as well as a compound that exceeds the activity of furosemide.

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Acute toxicity of 3-(2-, 3-fluorophenyl)-6-(aryl-, hetaryl)-[1,2,4]triazole[3,4-b][1,3,4]thiadiazoles

Abstract: Експериментальна та клінічна фармакологія Experimental and clinic pharmacology

Cited by 2 publications

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Synthesis and Biological Evaluation of New Schiff Bases Derived from 4-Amino-5-(3-fluorophenyl)-1,2,4-triazole-3-thione

Synthesis and Biological Evaluation of New Schiff Bases Derived from 4-Amino-5-(3-fluorophenyl)-1,2,4-triazole-3-thione

Diuretic activity of some 4- and 3-thio-substituted 1,2,4-triazoles with fluorophenyl fragments

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